Ultraflexible vesicles, Transfersomes, have an extremely low pore penetration resistance and transport therapeutic amounts of insulin across the intact mammalian skin.
New vehicles for the non-invasive delivery of agents are introduced. These carriers can transport pharmacological agents, including large polypeptides, through the permeability barriers, such as the intact skin. This capability depends on the self-regulating carrier deformability which exceeds that of the related but not optimized lipid aggregates by several orders of magnitude. Conventional lipid suspensions, such as standard liposomes or mixed lipid micelles, do not mediate a systemic biological effect upon epicutaneous applications. In contrast to this, the properly devised adaptable carriers, when administered on the intact skin, transport therapeutic amounts of biogenic molecules into the body. This process can be nearly as efficient as an injection needle, as seen from the results of experiments in mice and humans with the insulin-carrying vesicles. The carrier-mediated transcutaneous insulin delivery is unlikely to involve shunts, lesions or other types of skin damage. Rather than this, insulin is inferred to be transported into the body between the intact skin cells with a bio-efficiency of at least 50% of the s.c. dose action.
Cevc
G
G
Medical Biophysics, Clinics r.d.I., The Technical University of Munich, Germany.
Gebauer
D
D
Stieber
J
J
Schätzlein
A
A
Blume
G
G
D000279:Administration, Cutaneous; D000328:Adult; D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D002096:C-Peptide / Q000097:blood; D019826:Cholic Acid; D002793:Cholic Acids; D004337:Drug Carriers; D005260:Female; D006801:Humans; D007328:Insulin / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics; D008081:Liposomes / Q000737:chemistry*; D051379:Mice; D008815:Mice, Inbred Strains; D008823:Micelles; D010539:Permeability; D010713:Phosphatidylcholines; D051381:Rats; D011994:Recombinant Proteins; D012867:Skin / Q000378:metabolism*
D001786:Blood Glucose; D002096:C-Peptide; D002793:Cholic Acids; D004337:Drug Carriers; D007328:Insulin; D008081:Liposomes; D008823:Micelles; D010713:Phosphatidylcholines; D011994:Recombinant Proteins; D019826:Cholic Acid